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88 Cards in this Set
- Front
- Back
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omeprazole(Prilosec)
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PPI
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lansoprazole (Prevacid)
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PPI
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rebeprazole(Aciphex)
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PPI
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pantoprazole(Protonix)
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PPI
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esomeprazole (Nexium)
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PPI
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cimetidine(Tagamet)
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H2 receptor antagonist
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ranitidine (Zantac)
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H2 receptor antagonist
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famotidine (Pepcid)
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H2 receptor antagonist
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nizatidine (Axid)
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H2 receptor antagonist
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The H2 receptor upregulates the H+,K+ ATPase through which pathway?
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cAMP-dependent pathway
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PPI's are ________. That is, they must be activated in the body to inhibit the H+,K+ ATPase.
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prodrugs
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How are PPI's administered?
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orally
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The prodrug form of PPI's is a weak _____ and thus accumulates in the __________ cannaliculi of the parietal cell where it is activated by H+.
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The prodrug form of PPI's is a weak base and thus accumulates in the acidic cannaliculi of the parietal cell where it is activated by H+.
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Is PPI inactivation of the H+,K+ ATPase reversible?
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NO - PPI's irreversibly inactivate the H+, K+ ATPase
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How is the irreversible inhibition of the H+,K+ ATPase by a PPI overcome?
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synthesis of new proton pump proteins
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How are PPI's metabolized?
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cytochrome p450
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When should PPI's be taken?
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before or with a meal since food stimulates acid production
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Why should PPI's not be taken simultaneously with H2 receptor blockers?
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PPI's are prodrugs and need the acidic environment of the parietal cell cannaliculi for activation; the H2 receptor antagonist will block acid production needed to activate the PPI
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How do H2 receptor antagonists work?
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they reversibly compete with histamine for binding to the H2 receptor expressed on the basolateral surface of the parietal cell; thus they are competitive inhibitors of histamine stimulation of H+ produciton by parietal cells
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Where is the major source of histamine with which H2 receptor antagonists compete?
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enterochromaffin cells are the major source of histamine that binds the H2 receptor on the basolateral side of the parietal cell
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How does the potency of H2 receptor antagonist differ from PPI's?
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The primary effect of H2R antagonists is on basal H+ secretion (less effect on suppression of H+ secretion in response to feeding, gastrin, hypoglycemia, or vagal stimulation)
PPI's are significantly more potent and block up to 95% of H+ secretion |
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Why are H2R antagonists commonly prescribed to be taken before bedtime?
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inhibition of nocturnal H+ secretion is important for healing gastric and duodenal ulcers and H2R antagonists are very effective at inhibiting nocturnal H+ secretion
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What are the primary therapeutic indications for prescribing H2R antagonists?
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-promote healing of gastric and duodenal ulcers
-treatment of uncomplicated GERD -prophylaxis of stress ulcers |
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What are the primary therapeutic indications for Proton Pump Inhibitors?
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-Promote healing of gastric and duodenal ulcers
-Treat GERD (especially when unresponsive to H2R antagonists) -Treat Zollinger-Ellison syndrome |
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What are some of the side effects of PPI's?
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nausea, abdominal pain, constipation, flatulance, diarrhea
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What are some of the side effects of H2R antagonists?
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diarrhea, headache, drowsiness, fatigue, muscular pain, constipation
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What kind of drug is Misoprostol?
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a prostaglandin analog - decreases activity of H+,K+ ATPase
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Misoprostol works through which receptor? What does it do?
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Misoprostol is a prostaglandin analog.
In the parietal cell, it works through the EP3 receptor to downregulate the H+,K+ ATPase via a cAMP dependent pathway and thus decrease H+ secretion In the superficial epithelial cell, it works thru the EP3 receptor to stimulate mucus and bicarbonate secretion. |
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What are the indications for misoprostol?
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Misoprostol is used therapeutically to protect the gastric mucosa from injury in patients who are using NSAIDS for things like arthritis
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What does sucralfate do?
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they are a octasulfate of sucrose plus aluminum hydroxide - undergoes crosslinking in stomach to produce a viscous gel that adheres to and protects the stomach mucosa
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How is H. pylori infection treated?
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Combination therapies:
PPI + clarithromycin + amoxicillin or metronidazole PPI + bismuth + metronidazole + tetracycline |
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Which neuronal plexus regulates motor control in the GI tract?
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myenteric (Auerbach's) plexus - between circular and longitudinal muscle layers
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Which neuronal plexus regulates secretion, fluid transport, and vascular flow in the GI tract?
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submucosal (Meissner's) plexus
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What is the excitatory neurotransmitter of the myenteric plexus? Inhibitory?
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Excitatory - ACh
Inhibitory - Nitric Oxide (NO) |
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What role do interstitial cells of Cajal play in the gut?
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mediate neurogenic influence on GI smooth muscle (responsive to NO, ACh, and substance P)
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Why are cholinomimetic agents generally ineffective as prokinetic agents in the treatment of GI disorders?
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they act globally and cause uncoordinated contractions that are very much unlike the coordinated propulsion of peristalsis
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Carbachol
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muscarinic agonist - not used widely to treat GI disorders because it acts too globably and directly on GI smooth muscle producing uncoordinated motion
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Bethanechol
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muscarinic agonist - not used widely to treat GI disorders because it acts too globably and directly on GI smooth muscle producing uncoordinated motion
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Neostigmine
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Acetylcholinesterase inhibitor used to treat some GI disorders ass'd with pseudo-obstruction and paralytic ileus
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What role does dopamine have in the enteric nervous system?
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dopamine has several inhibitory effects on GI motility; suppresses ACh release
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Domperidone
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D2R antagonist - competitive inhibitor of dopamine receptor (dopamine inhibits ACh release thus decreasing GI motility)
NOT used in USA |
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What role does serotonin (5-HT) play in the GI tract?
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serotonin (5-HT) is found in neurons of the myenteric plexus and it modules secretion and motor activity
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Which serotonin (5-HT) receptors modulate GI tract motility?
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5HT3 (inhibitory)
5HT4 (excitatory) |
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Metoclopramide
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5-HT4 agonist and D2R antagonist
-functions primarily in the upper digestive tract -increases LES tone -taken po, used for gastric emptying -dopamine antagonism ameliorates nausea and vomiting in GI dysmotility syndromes |
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Zelnorm
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5-HT4 agonist
-FDA approved for IBS but withdrawn from market last year due to elevated risk of cardiac event |
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Octreotide
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somatostatin analog
-accelerates gastric emptying -inhibits release of hormones responsible for severe GI distress related to rapid passage of food in small bowel -used for decrease portal HTN in cases of variceal bleeding -can be used to treat severe secretory diarrhea caused by hormone-secreting tumors of the pancreas or GI tract |
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Erythromycin
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this macrolide antibiotic is a motilin (strong prokinetic hormone) receptor agonist with prokinetic activity
motlin receptors are located directly on GI smooth muscle |
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What is the chemo receptor-trigger zone (CTZ)?
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it is a part of the mid-brainstem that is adjacent to the site that coordinates emesis
it is OUTSIDE the blood-brain barrier which allows it to monitor for toxic substances |
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Ondansetron (Zofran)
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5-HT3 receptor antagonist
-treatment of chemo-induced emesis -also used for nausea related to upper abdominal irradiation and hyperemesis of pregnancy -NOT useful for motion sickness |
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Granisetron (Kytril)
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5-HT3 receptor antagonist
-treatment of chemo-induced emesis -also used for nausea related to upper abdominal irradiation and hyperemesis of pregnancy -NOT useful for motion sickness |
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Dolasteron (Anzemet)
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5-HT3 receptor antagonist
-treatment of chemo-induced emesis -also used for nausea related to upper abdominal irradiation and hyperemesis of pregnancy -NOT useful for motion sickness |
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Prochlorperazine
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-Phenothiazine
-antagonist of the dopamine D2 receptor at the CTZ -also have anti-histamine and anti-cholinergic activity -common antinauseant, antiemetic |
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Thiethylperazine
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-Phenothiazine
-antagonist of the dopamine D2 receptor at the CTZ -also have anti-histamine and anti-cholinergic activity -common antinauseant, antiemetic |
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Chlorpromazine
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-Phenothiazine
-antagonist of the dopamine D2 receptor at the CTZ -also have anti-histamine and anti-cholinergic activity -common antinauseant, antiemetic |
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Generally speaking, histamine H1 antagonists are indicated for.....
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-motion sickness
-postoperative emesis |
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Cyclizine
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-histamine H1 antagonist
-use for motion sickness or postoperative emesis |
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Hydroxyzine
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-histamine H1 antagonist
-use for motion sickness or postoperative emesis |
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Promethazine
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-histamine H1 antagonist
-use for motion sickness or postoperative emesis |
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Dipehenhydramine
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-histamine H1 antagonist
-use for motion sickness or postoperative emesis |
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Scopolamine
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-widely used anticholinergic antagonist
-can be administered as transdermal patch -used to prevent/treat motion sickness |
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Dronabinol
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-naturally occuring cannaboid
-used prophylactically as an antiemetic in patients receiving chemo when other antiemetics fail -also stimulates appetitie -mechanism not clearly understood |
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Glucocorticoids
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can be used as an antiemetic in patients with widespread cancer
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Psyllium (Metamucil)
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intraluminal, water-absorbing agent to treat diarrea
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Polycarbophil (FIBERCON, FIBERALL)
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intraluminal, water-absorbing agent to treat diarrea
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Carboxymethylcellulose
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intraluminal, water-absorbing agent to treat diarrea
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Kaolin and pectin (KAOPECTOLIN)
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intraluminal, water-absorbing agent to treat diarrea
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Attapulgite (DIASORB)
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intraluminal, water-absorbing agent to treat diarrea
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Cholestyramine (QUESTRAN)
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-anion exchange resin that binds bile acids and can also bind some bacterial toxins
-used to treat bile-salt induced diarrhea post resection of distal ileum -can also bind medications so should not be given within a few hours of another drug |
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Bismuth (PEPTO-BISMOL)
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-OTC antidiarrhetic
-antisecretory, antiinflammatory, and antimicrobial effects -relieves cramps and nausea -useful in treating H. pylori infection |
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Loperamide (Imodium)
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-increases small bowel transit time and sphincter tone
-OTC and useful for traveler's diarrhea |
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Dipenoxylate (Lomotil)
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-antidiarrheal
-related to meperidine -lots of CNS effects, can be addictive |
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Difenoxin (Motofen)
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-antidiarrheal
-related to meperidine -lots of CNS effects, can be addictive |
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Bran
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-effective anti-constipation agent
-increases stool volume, stretches wall of GI tract stimulating peristalsis |
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Polyethylene glycol (PEG)
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-used for constipation
-retains water in lumen of the GI tract |
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Sulfasalazine (Azulfidine)
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a 5-aminosalicylic acid linked to sulfapyridine
-oral use for mild/moderate ulcerative colitis -side effects: nausea, vomiting, heartburn, headache |
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Mesalamine (Asacol, Rowasa)
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inhibit COX and 5-lipoxygenase pathways
-used to treat IBD -fewer side effects than sulfasalazines -tablet po or rectally (enema or suppository) |
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Olsalazine (Dipentum)
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inhibit COX and 5-lipoxygenase pathways
-used to treat IBD -fewer side effects than sulfasalazines -tablet po or rectally (enema or suppository) |
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Balsalazide (Colazal)
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inhibit COX and 5-lipoxygenase pathways
-used to treat IBD -fewer side effects than sulfasalazines -tablet po or rectally (enema or suppository) |
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Glucocorticoids (in IBD)
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-potent anti-inflammatory agent
-major side effects -only use in moderate-severe IBD that doesn't respond to other therapy |
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Budesonide (Entocort EC)
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newer form of glucocorticoid used to treat IBD
-metabolized faster = less side effects |
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6-mercaptopurine (6-MP)
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Thioguanine derivative used in IBD to suppress lymphocyte proliferation and for its anti-inflammatory effects
-slow onset of action -major side effects |
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azathioprine (IMURAN, AZA)
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Thioguanine derivative used in IBD to suppress lymphocyte proliferation and for its anti-inflammatory effects
-slow onset of action -major side effects |
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Methotrexate
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Strong immune suppressant and anti-inflammatory that inhibits DHFR
-used to treat IBD among other things -major side effects |
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Cyclosporine (Sandimmune, Neoral)
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Calcineurin inhibitor, strong immunosuppressant and anti-inflammatory
-used for acute, severe ulcerative colitis -major side effects |
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Infliximab (REMICADE; cA2)
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monoclonal ab to TNF-alpha used to treat IBD (Crohn's and UC)
-IV injection -also used in children with moderate to severe Crohn's who haven't responded to other therapies -also used for: rheumatoid arthritis, ankylosing spondylitis, plaque psoriasis, psoriatic arthritis -can increase risk of infection (TB) -side effects: respiratory infections, headache, rash, cough, stomach pain -must NOT be taken with Anakinara (you don't want to take a TNF-alpha ab with an IL-1 inhibitor) |
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Adalimumab (HUMIRA, Abbott)
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monoclonal ab to TNF-alpha used to treat IBD (Crohn's and UC)
-subcu injection -also used for: rheumatoid arthritis, ankylosing spondylitis, plaque psoriasis, psoriatic arthritis -can increase risk of infection (TB) -side effects: respiratory infections, headache, rash, cough, stomach pain -must NOT be taken with Anakinara (you don't want to take a TNF-alpha ab with an IL-1 inhibitor) |
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ENBREL
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cytokine trap
-approved for: rheumatoid arthritis ankylosing spondylitis plaque psoriasis psoriatic arthritis juvenile rheumatoid arthritis |
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Natalizumab
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monoclonal ab against alpha-4 integrin
-blocks recruitment of immune cells to site of inflammation -being used in a select group of Crohn's disease and MS patients |
